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Tepotinib oral


Oral formulations of tepotinib.

Drugs List

  • TEPMETKO 225mg film coated tablets
  • tepotinib 225mg film coated tablets
  • Therapeutic Indications


    Advanced non-small cell lung cancer (NSCLC) with METex14 mutation

    Treatment of adult patients with advanced non-small cell lung cancer (NSCLC) harbouring mesenchymal-epithelial transition factor gene (MET) exon 14 (METex14) skipping alterations.



    450mg once daily.

    Additional Dosage Information

    Dose modifications for adverse reactions

    The recommended dose reduction for the management of adverse reactions is 225mg daily.

    Any grade interstitial lung disease (ILD)
    Withhold tepotinib if ILD is suspected. Permanently discontinue tepotinib if ILD is confirmed.

    Increased ALT and/or AST without increased total bilirubin
    Grade 3: Withhold tepotinib until recovery to baseline ALT/AST. If recovered to baseline within 7 days then resume tepotinib at the same dose, otherwise resume tepotinib at a reduced dose.
    Grade 4: Permanently discontinue tepotinib.

    Increased ALT and/or AST with increased total bilirubin in the absence of cholestasis or hemolysis
    ALT and/or AST greater than 3 x ULN with total bilirubin greater than 2 x ULN: Permanently discontinue tepotinib.

    Increased total bilirubin without concurrent increased ALT and/or AST
    Grade 3: Withhold tepotinib until recovery to baseline bilirubin. If recovered to baseline within 7 days then resume at a reduced dose, otherwise permanently discontinue.
    Grade 4: Permanently discontinue tepotinib.

    Other adverse reactions
    Grade 2: Maintain dose level. If intolerable, consider withholding tepotinib until resolved, then resume tepotinib at a reduced dose.
    Grade 3: Withhold tepotinib until resolved, then resume tepotinib at a reduced dose.
    Grade 4: Permanently discontinue tepotinib.

    Missed doses
    If a dose is missed, it should be taken as soon as remembered on the same day unless the next dose is due within 8 hours.


    Children under 18 years
    Renal impairment - creatinine clearance 15-29ml/minute
    Severe hepatic impairment

    Precautions and Warnings

    Glucose-galactose malabsorption syndrome
    Lactose intolerance

    Advise ability to drive/operate machinery may be affected by side effects
    Confirm METex14 mutation status prior to treatment
    Treatment to be initiated and supervised by a specialist
    Contains lactose
    Consult local policy on the safe use of oral anti-cancer drugs
    Staff: Not to be handled by pregnant staff
    Exclude pregnancy prior to initiation of treatment
    Monitor liver function before, every 2 weeks for 3 months & then monthly
    Advise patient to report any new or worsening respiratory symptoms
    Discontinue treatment if interstitial lung disease develops
    May affect results of some laboratory tests
    Discontinue if AST/ALT > 3 x ULN and bilirubin > 2 x ULN
    Discontinue permanently if AST or ALT level exceeds 20 x ULN
    Discontinue treatment if total bilirubin > 10 x ULN
    Interrupt therapy if elevations in bilirubin of > 3 x ULN occur
    Interrupt treatment if ALT or AST > 5 x ULN
    Suspend treatment if interstitial lung disease is suspected
    Permanently discontinue treatment if grade 4 adverse reactions occur
    Suspend treatment/reduce dose if grade 3 adverse reactions occur
    Advise patient not to take St John's wort concurrently
    Female: Contraception required during and for 1 week after treatment
    Male: Use of condoms required during and for 1 week after treatment
    Breastfeeding: Do not breastfeed during & for 1 week after treatment

    Interstitial lung disease (ILD)
    Patients should be monitored for new or worsening pulmonary symptoms. If ILD is suspected, then tepotinib should be withheld immediately whilst the patient is promptly investigated for alternative diagnosis or specific aetiology of ILD. Tepotinib must be permanently discontinued if ILD is confirmed.

    Pregnancy and Lactation


    Tepotinib is contraindicated during pregnancy.

    The manufacturer recommends that tepotinib is not used during pregnancy. There are no clinical data of the use of tepotinib in pregnant women. Studies in animals have shown teratogenicity and based on the mechanism of action and findings in animals, it is expected that tepotinib can cause foetal harm in pregnant women.


    Tepotinib is contraindicated during breastfeeding.

    The manufacturer recommends the breastfeeding should be discontinued during treatment with tepotinib and for at least 1 week after the last dose. There are no data regarding whether tepotinib or its metabolites are excreted in human milk, or its effects on the breast-fed infant or milk production.

    Side Effects

    Abdominal discomfort
    Abdominal pain
    Acute respiratory distress
    Alanine aminotransferase increased
    Aspartate aminotransferase increased
    Elevated amylase levels
    Elevated serum lipase
    Gastro-intestinal pain
    Hepatic pain
    Increase in alkaline phosphatase
    Increase in creatinine
    Interstitial lung disease

    Effects on Laboratory Tests

    Non-clinical studies suggest that tepotinib or its main metabolite inhibit the renal tubular transporter proteins, organic cation transporter (OCT) 2 and multidrug and toxin extrusion transporters (MATE) 1 and 2. Creatinine is a substrate of these two transporters and the observed increases in creatinine in these studies may be the result of the inhibition of active tubular secretion rather than renal impairment. Renal function tests that rely on serum creatinine should be interpreted with caution due to this effect of tepotinib. In cases of increased blood creatinine during tepotinib treatment, it is recommended that further assessment of the renal function should be performed to exclude renal impairment.


    It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

    The following number will direct the caller to the relevant local centre (0844) 892 0111

    Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( ) or if this is unavailable at the backup site ( ).

    Further Information

    Last Full Review Date: October 2021

    Reference Sources

    Summary of Product Characteristics: Tepmetko 225mg film-coated tablets. Merck Serono Ltd. Revised September 2021.

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    Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content

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